Bremelanotide is a melanocortin receptor agonist that has been approved by the FDA for the on-demand treatment of premenopausal women with systemic, acquired hypoactive sexual desire disorder (HSDD). Bremelanotide can be administered by intranasal or subcutaneous injection and has been shown to improve sexual desire, arousal, and orgasm scores. Since FDA approval, it has been primarily available to premenopausal women, but has been prescribed off-label to postmenopausal women and to men diagnosed with ED and other types of sexual dysfunction after a biopsychosocial assessment.

Bremelanotide is a centrally acting cyclic heptapeptide analog of the neuropeptide alpha-melanocyte stimulating hormone with high affinity for the melanocortin-4 receptor. Bremelanotide modulates dopaminergic pathways involved in sexual desire and arousal. In an fMRI study, Bremelanotide was shown to improve connectivity between the amygdala and insula during visual sexual stimulation, improve sexual brain processing, enhance cerebellum and supplementary motor area activity, and deactivate the secondary somatosensory cortex compared to placebo. Bremelanotide 1.75 mg/0.3 ml (Vyleesi?) was found to increase genital blood flow in both men and women within hours after subcutaneous injection via a disposable auto-injector. Its Phase 2 study was conducted in men with erectile dysfunction (ED). This suggests that Bremelanotide also has a certain therapeutic effect on male sexual dysfunction.

In addition, we analyzed the prescription patterns and renewal rates of off-label and off-label medications in male and female patients with various sexual dysfunctions over a 46-month period. The analysis included a breakdown of prescription dispensing for men, premenopausal women (categorized by age 18-50), and postmenopausal women (categorized by age >50), and further analyzed renewal and renewal rates. Bremelanotide has been used to treat a variety of sexual dysfunctions over a 46-month period: 76 bremelanotide prescriptions were dispensed in our clinic, 104 in postmenopausal women, and 444 in men. For premenopausal women, 29% of prescriptions were refills, for postmenopausal women, 52% were refills, and for men, 65% were refills. Refill rates within the past 18 months were 47% for premenopausal women (n = 30), 52% for postmenopausal women (n = 29), and 73% for men (n = 219). Refill rates and prescribing practices for any medication reflect, to some extent, the safety and efficacy of the treatment in a real-world setting. We observed an increase in bremelanotide refill rates for all patients. Notably, the refill rate was particularly high among male patients, suggesting that bremelanotide, a centrally acting drug, can be used as needed to successfully treat a variety of sexual dysfunctions.

References:

[1] AMBER N EDINOFF. Bremelanotide for Treatment of Female Hypoactive Sexual Desire.[J]. ACS Applied Electronic Materials, 2022: 75-88. DOI:10.3390/neurolint14010006.

[2] GOLDSTEIN I, GOLDSTEIN S. (227) Use of the CNS Agent Bremelanotide in Men with Sexual Dysfunction: Results from a Sexual Medicine Clinic[J]. The Journal of Sexual Medicine, 2024, 16 10. DOI:10.1093/jsxmed/qdae001.217.